Bioequivalence study of two formulations of terazosin hydrochloride capsule in healthy Chinese subjects under fasting and fed conditions

• Published in: International journal of clinical pharmacology and therapeutics Vol. 60; no. 1; pp. 57 - 66
• Main Authors: Fan, Lian-Lian, Li, Mu-Peng, Wu, Tong, Gan, Chun-Yan, Zhang, Pei-Wen, Mai, Gang, Shen-Tu, Jian-Zhong
• Format: Journal Article
• Language: English
• Published: Germany Dustri - Verlag Dr. Karl Feistle GmbH & Co. KG 01.01.2022
• Subjects: Adrenergic receptors; Area Under Curve; Bioequivalence; Blood pressure; China; Chromatography, Liquid; Clinical trials; Cross-Over Studies; Drug dosages; Fasting; Healthy Volunteers; Hepatitis; Hospitals; Humans; Hypertension; Infectious diseases; Laboratories; Medical diagnosis; Parkinson's disease; Pharmacokinetics; Pharmacy; Plasma; Prazosin - analogs & derivatives; Prostate; Smooth muscle; Tablets; Tandem Mass Spectrometry; Therapeutic Equivalency; China
• ISSN: 0946-1965
• DOI: 10.5414/CP204018

This study was conducted to assess the pharmacokinetic and safety profiles between a new oral formulation of terazosin hydrochloride capsule compared with the brand-name drug. A randomized, open-label, single-dose, 2-period crossover study under fasting or fed conditions was conducted in healthy Chinese subjects. 24 individuals were selected, respectively. Each subject was randomized at the beginning to receive a 2-mg capsule of the test or the reference terazosin during the first period and then received the alternate formulation during the second period following a 1-week washout period. Blood samples were collected at pre-dose and up to 60 hours after administration. Plasma terazosin was quantified by a validated LC-MS/MS method. 48 healthy subjects were enrolled, and 47 completed the study. C , AUC , and AUC were similar and the 90% CIs for the geometric mean ratios of these parameters between the two groups were all bounded within the predefined bioequivalence criterion of 80 - 125% under both fasting and fed conditions. Throughout the study period, a total of 30 treatment-emergent adverse events (TEAEs) were reported under fasting condition. 35 TEAEs were observed under fed conditions. No serious adverse event was observed. The test and reference formulations of terazosin were bioequivalent and well tolerated under both fasting and fed conditions.